HISTAMINE H1 RECEPTOR

Approval Year

Substance Class	Protein Created by `admin` on `Tue Apr 01 18:33:56 GMT 2025` Edited by `admin` on `Tue Apr 01 18:33:56 GMT 2025`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	28XBT591QG
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

HISTAMINE H1 RECEPTOR

Common Name

English

H1R

Preferred Name

English

HRH1

Common Name

English

Common Name

English

HH1R

Common Name

English

Code System Code Type Description

UNIPROT

P35367

Created by admin on Tue Apr 01 18:33:56 GMT 2025 , Edited by admin on Tue Apr 01 18:33:56 GMT 2025

PRIMARY

FDA UNII

28XBT591QG

Created by admin on Tue Apr 01 18:33:56 GMT 2025 , Edited by admin on Tue Apr 01 18:33:56 GMT 2025

PRIMARY

From	To
1_100	1_180
1_441	1_444

Glycosylation Type

HUMAN

Glycosylation Link Type	Site
N	1_5
N	1_18

Related Record Type Details


					3L5TQ84570

MECLIZINE

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Pyrilamine H-3

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Qualification:

Amount:


					L6UH7ZF8HC

RISPERIDONE

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Interaction Type:

INHIBITOR

Qualification:

Amount:


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LATREPIRDINE

INHIBITOR -> TARGET

Qualification:

IC50

Amount:


					95QB77JKPL

DOXYLAMINE

INHIBITOR -> TARGET


					820484N8I3

HISTAMINE

AGONIST -> TARGET

Comments:

CHO-H1 cells, histamine stimulation resulted in a concentration-dependent increase in [Ca2+]i with an EC50 of 170±30 nM.

Qualification:

EC50

Amount:


					BGL0JSY5SI

QUETIAPINE

INHIBITOR -> TARGET

Qualification:

Amount:


					SIG10953FN

BAMIRASTINE

INHIBITOR -> TARGET

Amount:


					42FZN61Y9L

NBI-2 (NON-LABELED)

INHIBITOR -> TARGET

Amount:


					Z5014VUX83

VAPITADINE

INHIBITOR -> TARGET

Amount:


					Z7XU1T6K9Q

NBI-2

INHIBITOR -> TARGET

Amount:


					LAH70H9JPH

TIAPRIDE

INHIBITOR -> TARGET


					E6582LOH6V

FEXOFENADINE

INHIBITOR -> TARGET


					3C5ORO99TY

TRIPELENNAMINE

INHIBITOR -> TARGET


					QRW9FCR9P2

CYCLIZINE

INHIBITOR -> TARGET


					244O1F90NA

MIZOLASTINE

INHIBITOR -> TARGET


					W5DCO14M05

TECASTEMIZOLE

INHIBITOR -> TARGET

Amount:


					UG7PAX5TS3

PF-05150122

INHIBITOR->OFF-TARGET

Qualification:

IC50

Amount:


					Y463242LY2

MEQUITAZINE

INHIBITOR -> TARGET


					ZX1CC585SV

NBI-1

INHIBITOR -> TARGET

Amount:


					J4CZH8D9EN

6-FLUORO-DMT

AGONIST -> TARGET

Amount:


					63J9EQ81YC

LY-2624803

INHIBITOR -> TARGET


					772BQ8KSST

PHENINDAMINE

INHIBITOR -> TARGET


					2AE8M83G3E

RUPATADINE

INHIBITOR -> TARGET


					D27V6190PM

OLOPATADINE

INHIBITOR -> TARGET


					3Q9Q0B929N

DEXCHLORPHENIRAMINE

INHIBITOR -> TARGET


					FF28EJQ494

PROMETHAZINE

INHIBITOR -> TARGET


					80061L1WGD

CIMETIDINE

AGONIST -> TARGET

Qualification:

IC50

Amount:


					94Z39NID6C

AZATADINE

INHIBITOR -> TARGET


					242Z0PM79Y

PROPIOMAZINE

INHIBITOR -> TARGET


					EJG9C09D7R

NBI-75043

INHIBITOR -> TARGET

Amount:


					ZQI909440X

AZELASTINE

INHIBITOR -> TARGET


					K65LB6598J

PHENYLTOLOXAMINE

INHIBITOR -> TARGET


					2YHB6175DO

CYPROHEPTADINE

INHIBITOR -> TARGET


					733HOW0WT3

NBI-4

INHIBITOR -> TARGET

Amount:


					7HU6337315

ASTEMIZOLE

INHIBITOR -> TARGET


					U42B7VYA4P

CHLORPROMAZINE

INHIBITOR -> TARGET


					B6C301298G

EFLETIRIZINE

INHIBITOR -> TARGET

Amount:


					838F01T721

PALIPERIDONE

INHIBITOR -> TARGET

Interaction Type:

INHIBITOR

Qualification:

Amount:


					30S50YM8OG

HYDROXYZINE

INHIBITOR -> TARGET


					H57G17P2FN

BROMPHENIRAMINE

INHIBITOR -> TARGET


					HH0KD7Z416

EMBRAMINE

INHIBITOR -> TARGET


					TC6VTE3B6X

SUN-1334

INHIBITOR -> TARGET

Amount:


					2U5SUQ9CWU

NBI-4 (NON-LABELED)

INHIBITOR -> TARGET

Amount:


					BC73A8YT4A

REN-1869

INHIBITOR -> TARGET

Amount:


					668QM8QJFS

TAGORIZINE

INHIBITOR -> TARGET

Amount:


					75T64B71RP

DEXBROMPHENIRAMINE

INHIBITOR -> TARGET


					A051Q2099Q

MIRTAZAPINE

INHIBITOR -> TARGET


					51Z4H26U4W

NBI-3

INHIBITOR -> TARGET

Amount:


					S08212J4ZR

GSK-1004723

INHIBITOR -> TARGET

Comments:

Long acting slowly dissociates.

Interaction Type:

BINDING

Qualification:

Amount:


					4685R51V7M

ESMIRTAZAPINE

INHIBITOR -> TARGET

Amount:


					134FM9ZZ6M

PHENIRAMINE

INHIBITOR -> TARGET


					AL805O9OG9

ORPHENADRINE

INHIBITOR -> TARGET


					TQD7Q784P1

EBASTINE

INHIBITOR -> TARGET


					Q13WX941EF

EPINASTINE

ANTAGONIST->TARGET


					JB937PER5C

DIMENHYDRINATE

INHIBITOR -> TARGET


					V3H1ZVV9S6

Norquetiapine

INHIBITOR -> TARGET

Qualification:

Amount:


					62LN840SFZ

MAPINASTINE

INHIBITOR -> TARGET

Amount:


					0C94V6X681

BUCLIZINE

INHIBITOR -> TARGET


					8GTS82S83M

DIPHENHYDRAMINE

INHIBITOR -> TARGET


					982A7M02H5

CARBINOXAMINE

INHIBITOR -> TARGET


					YO7261ME24

CETIRIZINE

INHIBITOR -> TARGET


					5ASJ6HUZ7D

DOXEPIN

INHIBITOR -> TARGET


					FVF865388R

Desloratadine

INHIBITOR -> TARGET


					7Z8O94ECSX

ALCAFTADINE

AGONIST -> TARGET

Comments:

Alcaftadine is a H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells.


					6U5EA9RT2O

LEVOCETIRIZINE

INHIBITOR -> TARGET


					WQ8PCH72SD

NBI-3 (NON-LABELED)

INHIBITOR -> TARGET

Amount:


					3U6IO1965U

CHLORPHENIRAMINE

INHIBITOR -> TARGET


					661FH77Z3P

DIMETHINDENE

INHIBITOR -> TARGET


					95QN29S1ID

CLEMASTINE

INHIBITOR -> TARGET


					9BC2MUG4A8

AZD-3778

INHIBITOR -> TARGET

Amount:


					2L8T9S52QM

TRIPROLIDINE

INHIBITOR -> TARGET


					HPE317O9TL

PYRILAMINE

INHIBITOR -> TARGET


					5HML8P3QAT

UR-AK49

AGONIST -> TARGET

Amount:


					A20F9XAI7W

ACRIVASTINE

TARGET -> INHIBITOR


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LEVOMEQUITAZINE

INHIBITOR -> TARGET

Comments:

Binds stronger than R-isomer


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BEPOTASTINE

INHIBITOR -> TARGET


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BILASTINE

INHIBITOR -> TARGET


					7AJO3BO7QN

LORATADINE

INHIBITOR -> TARGET


					T032BI7727

BROMODIPHENHYDRAMINE

INHIBITOR -> TARGET

Structural Modifications

Modification Type	Location Site	Location Type	Residue Modified	Extent	Fragment Name	Fragment Approval
AMINO ACID SUBSTITUTION	[1_140] [1_142] [1_279]				THREONINE PHOSPHATE	3L4WX7B1EI
AMINO ACID SUBSTITUTION	[1_344] [1_347] [1_380] [1_396] [1_398]				DEXFOSFOSERINE	VI4F0K069V

Name	Property Type	Amount	Referenced Substance	Defining	Parameters	References
MOL_WEIGHT	CHEMICAL
Molecular Formula	CHEMICAL